.cp_wz table {border-top: 1px solid #ccc; border-left: 1px solid #ccc; } .cp_wz table td {border-right: 1px solid #ccc; borda inferior: 1px sólido #ccc; preenchimento: 5px 0px 0px 5px;} .cp_wz tabela th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; preenchimento: 5px 0px 0px 5px;} \ n Peso molecular: \ n 327,12 A niclosamida pode inibir a replicação do DNA e inibir o STAT com IC50 de 0,7 μM. \ n Atividade biológica Niclosamida (a niclosamida é capaz de inibir a replicação do SARS-CoV em uma concentração micromolar em Células Vero E6 infectadas com SARS-CoV. Niclosamida (Niclosamida inibe a atividade repórter NF-κB induzida por TNF de uma maneira dependente da dose e do tempo em células U2OS. A niclosamida (125 nM) inibe a ativação de NF-κB induzida por p65, IKKα , IKKβ, IKKγ e TAK1 em células U2OS. Niclosamida (40 mg / kg / d, ip) inibe o crescimento de células AML xenoenxertadas em camundongos nus com tumores de xenoenxerto HL-60. Protocolo (Apenas para Referência) Ensaio de Quinase: [1]
|
Protein Kinase profiling assay
|
Assay for 22 different proteins kinases is carried out by ProQinase Gmbh. All of the protein kinases are expressed either in Sf9 insect cells or in E.coli as recombinant GST-fusion proteins or His-tagged proteins. Protein kinases are purified by affinity chromatography using either GSH-agarose or Ni_NTH-agarose. A radiometric protein kinase assay is used for measuring the kinase activity of the 22 protein kinases. Briefly, for each protein kinase, 50 μL reaction cocktail containing 60 mM HEPES-NaOH, 3 mM MgCl2, 3 mM MnCl2, 3 μM Na-orthovanadate, 1.2 mM DTT, 50 μg/mL PEG20000, 1 μM [γ-33P]-ATP, Niclosamide, adequate amount of enzyme and its substrate. The PKC-alpha assay additionally contain 1 mM Cacl2, 4 mM EDTA, 5 μg/mL phosphatidylserine and 1 μg/mL 1, 2-Dioleyl-glycerol. The reaction cocktails are incubated at 37 °C for 60 minutes and stop with 50 μL 2% (v/v) H3PO4. Incorporation of 33Pi is determined with a microplate scintillation counter. The activities and the IC50 values are calculated using Quattro Workflow V2.28.
|
Ensaio de células: [1]
|
Cell lines
|
Hela, A549, Du145, HT-29, A431, PC3 cells
|
|
Concentrations
|
16 μM
|
|
Incubation Time
|
72 hours
|
|
Method
|
Cells are plated in 96-well culture plates with cell density of 3-4 × 103 cells/well and treat with Niclosamide by adding 100 μL medium containing Niclosamide of various concentrations on the second day. After 72-hour's treatment, MTT is added to each well and incubated for additional 4-5 hours, and the absorbance is measured on a microplate reader at 570nm. Cell growth inhibition is evaluated as the ratio of the absorbance of the sample to that of the control. The results are representative of at least 3 independent experiments.
|
Estudo Animal: [4]
|
Animal Models
|
nude mice bearing HL-60 xenograft tumors.
|
|
Formulation
|
DMSO
|
|
Dosages
|
40 mg/kg
|
|
Administration
|
Intraperitoneal injection
|
|
Solubility
|
1% DMSO/30% polyethylene glycol/1% Tween 80,
30 mg/mL
|
|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|
Conversão de diferentes modelos de animais com base em BSA (valor com base em dados das diretrizes preliminares da FDA)
|
Species
|
Baboon
|
Dog
|
Monkey
|
Rabbit
|
Guinea pig
|
Rat
|
Hamster
|
Mouse
|
|
Weight (kg)
|
12
|
10
|
3
|
1.8
|
0.4
|
0.15
|
0.08
|
0.02
|
|
Body Surface Area (m2)
|
0.6
|
0.5
|
0.24
|
0.15
|
0.05
|
0.025
|
0.02
|
0.007
|
|
Km factor
|
20
|
20
|
12
|
12
|
8
|
6
|
5
|
3
|
|
Animal A (mg/kg) = Animal B (mg/kg) multiplied by
|
Animal B Km
|
|
Animal A Km
|
Por exemplo, para modificar a dose de resveratrol usada para um camundongo (22,4 mg / kg) para uma dose baseada na BSA para um rato, multiplique 22,4 mg / kg pelo fator Km para um camundongo e, em seguida, divida pelo fator Km para um rato. Este cálculo resulta em uma dose equivalente de rato para o resveratrol de 11,2 mg / kg.
|
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
|
mouse Km(3)
|
= 11.2 mg/kg
|
|
rat Km(6)
|
Informação Química
|
Molecular Weight (MW)
|
327.12
|
|
Formula
|
C13H8Cl2N2O4
|
|
CAS No.
|
50-65-7
|
|
Storage
|
3 years -20℃Powder
|
|
6 months-80℃in solvent (DMSO, water, etc.)
|
|
Synonyms
|
Niclocide
|
|
Solubility (25°C) *
|
In vitro
|
DMSO
|
<1 mg/mL
(
|
|
Water
|
<1 mg/mL
(
|
|
Ethanol
|
<1 mg/mL
(
|
|
In vivo
|
1% DMSO/30% polyethylene glycol/1% Tween 80
|
30 mg/mL
|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|
|
Chemical Name
|
Benzamide, 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-
|
Calculadora de molaridade Calculadora de diluição Calculadora de peso molecular
Grupo de Produto : JAK / STAT > Inibidor STAT
